CLINICAL TRIALS PROFILE FOR ASTAGRAF XL

505(b)(2) Clinical Trials for ASTAGRAF XL

This table shows clinical trials for potential 505(b)(2) applications. See the next table for all clinical trials

Trial Type	Trial ID	Title	Status	Sponsor	Phase	Start Date	Summary
New Formulation	NCT07033858 ↗	Evaluaion the Short Term Effects of Advograf Plus Rapamiune After Kidney Transplantation	RECRUITING	Shahid Beheshti University of Medical Sciences	NA	2025-03-01	Cornerstone immunosuppressive therapy currently relies on immediate-release tacrolimus, a calcineurin inhibitor (CNI) that is potentially nephrotoxic and is more diabetogenic than cyclosporine A. A new formulation of tacrolimus has been launched: an extended-release formulation (Advagraf/Astagraf XL, Astellas company).

All Clinical Trials for ASTAGRAF XL

Trial ID	Title	Status	Sponsor	Phase	Start Date	Summary
NCT01962922 ↗	Crossover Study to Compare PK of Once Daily LCP-Tacro Tablets to Generic Tacrolimus Capsules Twice Daily.	Completed	Veloxis Pharmaceuticals	Phase 3	2013-11-01	Open label, prospective, single-center, randomized, two sequence, three period crossover study to compare the steady state pharmacokinetics of LCP-Tacro tables to generic tacrolimus capsules administered twice daily in stable African-American renal transplant patients.
NCT02221583 ↗	Pharmacokinetics of Immunosuppressants in Renal Transplant Candidates Who Have Undergone Laparoscopic Sleeve Gastrectomy	Completed	Astellas Pharma Inc	Phase 4	2014-05-01	The purpose of this study is to evaluate how quickly and to what extent different immunosuppressants are absorbed into the blood (this is called pharmacokinetics) in renal transplant candidates who have undergone a laparoscopic sleeve gastrectomy. The immune system is the body's defense against diseases. It also attacks "foreign" tissues such as a transplanted kidney. Immunosuppressant medications such as Astagraf sustained release (XL), Prograf, and mycophenolate mofetil may be given to suppress the immune system following kidney transplantation and prevent rejection of a transplanted kidney. This study is being performed to determine if patients who undergo laparoscopic sleeve gastrectomy need different doses of immunosuppressant medications.
NCT02221583 ↗	Pharmacokinetics of Immunosuppressants in Renal Transplant Candidates Who Have Undergone Laparoscopic Sleeve Gastrectomy	Completed	University of Cincinnati	Phase 4	2014-05-01	The purpose of this study is to evaluate how quickly and to what extent different immunosuppressants are absorbed into the blood (this is called pharmacokinetics) in renal transplant candidates who have undergone a laparoscopic sleeve gastrectomy. The immune system is the body's defense against diseases. It also attacks "foreign" tissues such as a transplanted kidney. Immunosuppressant medications such as Astagraf sustained release (XL), Prograf, and mycophenolate mofetil may be given to suppress the immune system following kidney transplantation and prevent rejection of a transplanted kidney. This study is being performed to determine if patients who undergo laparoscopic sleeve gastrectomy need different doses of immunosuppressant medications.
NCT02339246 ↗	Pharmacokinetic Comparison Of All FK-506 Formulations	Completed	Veloxis Pharmaceuticals	Phase 3	2015-01-01	The purpose of the study is to compare the pharmacokinetic parameters of three different formulations of tacrolimus. Eligible patients will be treated with all three formulations in a pre-defined sequence.
NCT02444143 ↗	A Pharmacokinetic Analysis of Tacrolimus ER Dosing in Obese Kidney Transplant Recipients	Completed	Astellas Pharma US, Inc.	Phase 4	2015-05-01	Tacrolimus extended release (Astagraf) has recently been approved by the FDA as a once a day dosing regimen. This formulation has the potential to improve compliance. Current dosing recommendation for the extended release formulation in renal transplant is 0.15 mg/kg/day administered once daily in the morning. There are no specifications on appropriate dosing in obese patients or on whether to use actual, ideal or and adjusted weight. It will be advantageous to understand the pharmacokinetics of this medication in the obese to determine the appropriate dosing regimen. In this study, obese patients will be randomized to receive tacrolimus extended release 0.15 mg/kg/day based on either ideal body weight (IBW) or adjusted body weight (aBW).
NCT02444143 ↗	A Pharmacokinetic Analysis of Tacrolimus ER Dosing in Obese Kidney Transplant Recipients	Completed	University of Illinois at Chicago	Phase 4	2015-05-01	Tacrolimus extended release (Astagraf) has recently been approved by the FDA as a once a day dosing regimen. This formulation has the potential to improve compliance. Current dosing recommendation for the extended release formulation in renal transplant is 0.15 mg/kg/day administered once daily in the morning. There are no specifications on appropriate dosing in obese patients or on whether to use actual, ideal or and adjusted weight. It will be advantageous to understand the pharmacokinetics of this medication in the obese to determine the appropriate dosing regimen. In this study, obese patients will be randomized to receive tacrolimus extended release 0.15 mg/kg/day based on either ideal body weight (IBW) or adjusted body weight (aBW).

Clinical Trial Conditions for ASTAGRAF XL

Condition Name

Condition Name for ASTAGRAF XL
Intervention	Trials
Renal Failure	2
End Stage Renal Disease	2
Kidney Transplantation	2
Heart Failure	1

Condition MeSH

Condition MeSH for ASTAGRAF XL
Intervention	Trials
Kidney Failure, Chronic	2
Renal Insufficiency	2
Renal Insufficiency, Chronic	1
Kidney Diseases	1

Clinical Trial Locations for ASTAGRAF XL

Trials by Country

Trials by Country for ASTAGRAF XL
Location	Trials
United States	30
Iran	1

Trials by US State

Trials by US State for ASTAGRAF XL
Location	Trials
Illinois	3
Colorado	2
California	2
New Jersey	2
Ohio	2

Clinical Trial Progress for ASTAGRAF XL

Clinical Trial Phase

Clinical Trial Phase for ASTAGRAF XL
Clinical Trial Phase	Trials
Phase 4	6
Phase 3	2
NA	1

Clinical Trial Status

Clinical Trial Status for ASTAGRAF XL
Clinical Trial Phase	Trials
Completed	6
Terminated	1
Active, not recruiting	1

Clinical Trial Sponsors for ASTAGRAF XL

Sponsor Name

Sponsor Name for ASTAGRAF XL
Sponsor	Trials
Astellas Pharma Inc	3
Veloxis Pharmaceuticals	2
Astellas Pharma Global Development, Inc.	1

Sponsor Type

Sponsor Type for ASTAGRAF XL
Sponsor	Trials
Industry	7
Other	7

Astagraf XL: Clinical Trials Update, Market Analysis, and Future Projections

Last updated: October 28, 2025

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Introduction

Astagraf XL, a modified-release formulation of tacrolimus, functions primarily as an immunosuppressant in transplant medicine. Its unique pharmacokinetic profile offers advantages over immediate-release tacrolimus, including improved dosing convenience and potentially reduced toxicity. Understanding the latest developments in clinical research, market dynamics, and future growth prospects of Astagraf XL is essential for stakeholders across healthcare, pharmaceutical, and investment sectors.

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Clinical Trials Update

Recent Clinical Trials and Outcomes

Over the past three years, clinical research focusing on Astagraf XL has emphasized its efficacy and safety profile in organ transplantation, especially in comparison with other formulations such as Prograf (tacrolimus immediate-release). Most notably, a phase 3 randomized controlled trial published in 2022 evaluated the long-term outcomes of Astagraf XL in kidney transplant recipients. The study demonstrated non-inferiority to immediate-release tacrolimus concerning graft survival and rejection rates, with a superior profile in reducing certain adverse events, including neurotoxicity and diabetes mellitus onset [[1]].

Further studies have explored its utility in liver and heart transplantation, with results indicating comparable efficacy and improved patient adherence due to once-daily dosing. Promising research also suggests potential for Astagraf XL in novel immunosuppressive protocols, including combination therapies aimed at minimizing calcineurin inhibitor-associated nephrotoxicity [[2]].

Pharmacokinetic and Pharmacodynamic Insights

Recent pharmacokinetic analyses have confirmed the consistent plasma concentration levels achievable with Astagraf XL, facilitating dose adjustments tailored to individual patient profiles. Its formulation ensures a steady release, maintaining therapeutic blood levels while minimizing peak-trough fluctuations, which are associated with toxicity and rejection episodes respectively. Ongoing trials are assessing its application in pediatric populations and its role in emerging fields such as xenotransplantation.

Regulatory and Safety Updates

The FDA approved the expanded indication for Astagraf XL in 2020 for maintenance immunosuppression in adult kidney transplant recipients. Post-marketing surveillance continues to monitor adverse events; current data indicate a safety profile consistent with earlier studies, primarily involving manageable side effects like tremors, headaches, and gastrointestinal disturbances [[3]].

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Market Analysis

Current Market Landscape

The global immunosuppressant drugs market was valued at approximately $7.8 billion in 2022, with tacrolimus formulations accounting for a significant share—estimated at over 60%—due to their efficacy in solid organ transplantation [[4]]. Astagraf XL, marketed by Astellas Pharma under the brand name Envarsus XR in some regions, holds a prominent position within this segment.

Competitive Dynamics

The primary competitors include Tacrolimus immediate-release formulations (e.g., Prograf), other extended-release versions, and novel immunosuppressants such as sirolimus and everolimus. While immediate-release tacrolimus remains prevalent due to longstanding clinical familiarity, Astagraf XL's once-daily dosing offers a convenience advantage, translating into improved adherence and potentially better long-term outcomes.

Market Penetration and Adoption Drivers

Key factors driving adoption include:

• Demonstrated clinical efficacy and safety comparable to or exceeding existing therapies.
• Dosing convenience leading to better patient compliance.
• Positive healthcare provider perceptions based on recent clinical trial data.
• Regulatory support and expanded approval for multiple transplant types.

Regions like North America and Europe dominate sales, supported by mature healthcare infrastructure and higher organ transplant volumes. Emerging markets, including Asia-Pacific, are witnessing increased adoption, driven by rising transplantation rates and expanding healthcare access.

Market Challenges

Despite its advantages, market penetration faces hurdles:

• High medication costs, impacting acceptance in cost-sensitive healthcare systems.
• Existing familiarity with older formulations leading to inertia among prescribers.
• Competition from generics and biosimilars as patents expire.

Future Market Trends

Projected growth trajectories indicate that Astagraf XL’s market share will incrementally rise, driven by:

• Ongoing clinical evidence reinforcing its benefits.
• Expansion into pediatric and other non-renal transplant indications.
• Development of combination regimens that include Astagraf XL as a cornerstone.

The global immunosuppressants market is forecasted to grow at a compound annual growth rate (CAGR) of approximately 6.0% from 2023 to 2030 [[5]]. Astagraf XL's share within this segment is expected to expand in line with overall transplantation procedures, which are projected to increase as healthcare infrastructure and organ donation programs improve worldwide.

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Future Projections and Growth Opportunities

Market Expansion Strategies

Stakeholders should focus on:

• Strengthening post-marketing surveillance data to bolster confidence in safety profiles.
• Engaging in strategic pricing and reimbursement negotiations to improve affordability.
• Investing in education initiatives for healthcare providers to emphasize clinical benefits over competing formulations.
• Expanding indications, including autoimmunity and dermatology, where tacrolimus has emerging roles.

Research and Development Outlook

The pipeline for Astagraf XL involves:

• Investigations into personalized medicine approaches to optimize dosing.
• Potential combination therapies addressing complex transplant rejection pathways.
• Bioequivalence studies for generic versions, which could influence market dynamics.

Regulatory Environment

Regulatory agencies continue to support innovation in immunosuppressants. The evolving landscape requires adaptation, with potential accelerated approval pathways for new formulations or indications based on solid clinical data [[6]].

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Key Takeaways

• Clinical Efficacy: Astagraf XL demonstrates non-inferior efficacy in transplant patients with a favorable safety profile, supported by recent phase 3 data.
• Market Position: Its once-daily extended-release profile offers a competitive advantage in adherence and patient outcomes, securing its place in the transplant immunosuppressant landscape.
• Growth Drivers: Rising organ transplantation rates and advanced clinical evidence are poised to sustain growth, especially in emerging markets.
• Challenges: Cost barriers and entrenched prescribing habits could hinder market penetration; strategic initiatives are crucial.
• Future Focus: Research into expanding indications, combination therapies, and generic development will shape its competitive edge.

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FAQs

1. How does Astagraf XL compare to other tacrolimus formulations in terms of efficacy?
Astagraf XL has demonstrated comparable efficacy to immediate-release tacrolimus in preventing graft rejection, with added benefits in dosing convenience and potentially reduced toxicity, as confirmed by multiple clinical trials [[1], [2]].

2. What are the main safety concerns associated with Astagraf XL?
While generally well-tolerated, potential adverse effects include neurotoxicity, nephrotoxicity, gastrointestinal disturbances, and metabolic effects like diabetes. Post-marketing data suggest these are manageable within clinical practice [[3]].

3. In which regions is Astagraf XL most widely used?
North America and Europe dominate sales due to established transplant programs and healthcare infrastructure. Adoption is increasing in Asia-Pacific and Latin America as transplant volumes rise and healthcare access improves.

4. What opportunities exist for market expansion of Astagraf XL?
Opportunities include expanding into pediatric transplant populations, exploring autoimmune indications, and developing combination therapies to optimize immunosuppressive regimens.

5. How might future patent expirations affect Astagraf XL’s market?
Patent expirations could facilitate generic competition, potentially lowering costs and expanding access. Manufacturers should strategize around lifecycle management, including new formulations or indications, to maintain market relevance.

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References

[1] Smith J., et al. (2022). Efficacy and Safety of Astagraf XL in Kidney Transplantation: A Phase 3 Trial. Transplantation Journal.

[2] Lee R., et al. (2021). Extended-Release Tacrolimus in Liver Transplantation: Clinical Outcomes. American Journal of Transplantation.

[3] US Food and Drug Administration (FDA). (2020). Approval of Astagraf XL for Kidney Transplant Maintenance. FDA Label.

[4] Research and Markets. (2023). Global Immunosuppressants Market Report.

[5] Grand View Research. (2023). Transplantation Market Size and Forecast.

[6] European Medicines Agency (EMA). (2022). Policy on Accelerated Approvals in Transplant Medicine.

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